One-pot high-throughput synthesis of a 160-membered library of methyl 3,5-diaryl-isoxazoline-5-carboxylate pharmacophores by a 2·2·2-component reaction.

A simple and efficient methodology has been developed for the synthesis of methyl 3,5-diaryl-isoxazoline-5-carboxylates in a high-throughput fashion. This was accomplished in one-pot by a sequence of three 2-component reactions steps (2·2·2-CR), whereby compounds were obtained in overall 30-66% isolated yields. The functional group diversity was established by synthesizing a 160-membered library.